ME03392B - Prodrug derivatives of (e)-n-methyl-n-((3-methylbenzofuran-2-yl)methyl)-3-(7-oxo-5,6,7,8-tetrahydro-1,8-naphthyridin-3-yl)acrylamide - Google Patents

Prodrug derivatives of (e)-n-methyl-n-((3-methylbenzofuran-2-yl)methyl)-3-(7-oxo-5,6,7,8-tetrahydro-1,8-naphthyridin-3-yl)acrylamide

Info

Publication number
ME03392B
ME03392B MEP-2019-159A MEP2019159A ME03392B ME 03392 B ME03392 B ME 03392B ME P2019159 A MEP2019159 A ME P2019159A ME 03392 B ME03392 B ME 03392B
Authority
ME
Montenegro
Prior art keywords
methyl
methylbenzofuran
naphthyridin
tetrahydro
acrylamide
Prior art date
Application number
MEP-2019-159A
Other languages
German (de)
French (fr)
Unknown language (me)
Inventor
John J Partridge
John Colucci
Yves Gareau
Michel Therien
Robert Zamboni
Barry Hafkin
Anthony Marfat
Helmi Zaghdane
Original Assignee
Debiopharm Int Sa
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Debiopharm Int Sa filed Critical Debiopharm Int Sa
Publication of ME03392B publication Critical patent/ME03392B/en

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic System
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6561—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/66—Phosphorus compounds
    • A61K31/675—Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic System
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/553—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having one nitrogen atom as the only ring hetero atom
    • C07F9/576—Six-membered rings
    • C07F9/58—Pyridine rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic System
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/553—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having one nitrogen atom as the only ring hetero atom
    • C07F9/576—Six-membered rings
    • C07F9/60—Quinoline or hydrogenated quinoline ring systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/66—Phosphorus compounds
    • A61K31/662—Phosphorus acids or esters thereof having P—C bonds, e.g. foscarnet, trichlorfon

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Biochemistry (AREA)
  • Molecular Biology (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Pulmonology (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Diabetes (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicinal Preparation (AREA)
MEP-2019-159A 2012-06-19 2013-06-19 Prodrug derivatives of (e)-n-methyl-n-((3-methylbenzofuran-2-yl)methyl)-3-(7-oxo-5,6,7,8-tetrahydro-1,8-naphthyridin-3-yl)acrylamide ME03392B (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201261661559P 2012-06-19 2012-06-19
EP13806968.7A EP2861608B8 (en) 2012-06-19 2013-06-19 Prodrug derivatives of (e)-n-methyl-n-((3-methylbenzofuran-2-yl)methyl)-3-(7-oxo-5,6,7,8-tetrahydro-1,8-naphthyridin-3-yl)acrylamide
PCT/IB2013/001780 WO2013190384A1 (en) 2012-06-19 2013-06-19 Prodrug derivatives of (e)-n-methyl-n-((3-methylbenzofuran-2-yl)methyl)-3-(7-oxo-5,6,7,8-tetrahydro-1,8-naphthyridin-3-yl)acrylamide

Publications (1)

Publication Number Publication Date
ME03392B true ME03392B (en) 2020-01-20

Family

ID=49768192

Family Applications (1)

Application Number Title Priority Date Filing Date
MEP-2019-159A ME03392B (en) 2012-06-19 2013-06-19 Prodrug derivatives of (e)-n-methyl-n-((3-methylbenzofuran-2-yl)methyl)-3-(7-oxo-5,6,7,8-tetrahydro-1,8-naphthyridin-3-yl)acrylamide

Country Status (34)

Country Link
US (2) US8901105B2 (en)
EP (1) EP2861608B8 (en)
JP (2) JP6085026B2 (en)
KR (1) KR101720885B1 (en)
CN (1) CN104684922B (en)
AU (1) AU2013279021C1 (en)
BR (2) BR112014031635B1 (en)
CA (1) CA2875916C (en)
CL (1) CL2014003472A1 (en)
CY (1) CY1122006T1 (en)
DK (1) DK2861608T3 (en)
EA (1) EA028136B1 (en)
ES (1) ES2731474T3 (en)
HK (1) HK1208226A1 (en)
HR (1) HRP20190980T1 (en)
HU (1) HUE043836T2 (en)
IL (1) IL236066A (en)
IN (1) IN2014KN02915A (en)
LT (1) LT2861608T (en)
MA (1) MA37625B1 (en)
ME (1) ME03392B (en)
MX (1) MX356695B (en)
MY (1) MY170437A (en)
NZ (1) NZ702695A (en)
PH (1) PH12014502823B1 (en)
PL (1) PL2861608T3 (en)
PT (1) PT2861608T (en)
RS (1) RS58898B1 (en)
SG (1) SG11201408100YA (en)
SI (1) SI2861608T1 (en)
TN (1) TN2014000506A1 (en)
TR (1) TR201909016T4 (en)
UA (1) UA113215C2 (en)
WO (1) WO2013190384A1 (en)

Families Citing this family (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2008009122A1 (en) 2006-07-20 2008-01-24 Affinium Pharmaceuticals, Inc. Acrylamide derivatives as fab i inhibitors
SI2861608T1 (en) 2012-06-19 2019-08-30 Debiopharm International Sa Prodrug derivatives of (e)-n-methyl-n-((3-methylbenzofuran-2-yl)methyl)-3-(7-oxo-5,6,7,8-tetrahydro-1,8-naphthyridin-3-yl)acrylamide
CA3014541A1 (en) 2016-02-26 2017-08-31 Debiopharm International S.A. Medicament for treatment of diabetic foot infections
WO2018048882A1 (en) 2016-09-06 2018-03-15 The Research Foundation For The State University Of New York Positron imaging tomography imaging agent composition and method for bacterial infection
PE20211202A1 (en) 2017-08-24 2021-07-05 Novo Nordisk As COMPOSITIONS OF GLP-1 AND ITS USES
WO2019177975A1 (en) * 2018-03-12 2019-09-19 The Board Of Trustees Of The University Of Illinois Antibiotics effective for gram-negative pathogens
AU2019380568A1 (en) 2018-11-12 2021-06-17 Debiopharm International S.A. Antibiotic compounds, methods of manufacturing the same, pharmaceutical compositions containing the same and uses thereof
CN113507929A (en) 2018-12-21 2021-10-15 阿科利斯制药有限责任公司 DNA polymerase IIIC inhibitor and application thereof
EA202192246A1 (en) 2019-02-14 2021-11-18 Дебиофарм Интернэшнл C.A. COMPOSITION WITH APHABICIN, METHOD OF ITS PREPARATION AND ITS APPLICATION
BR112021025306A8 (en) * 2019-06-14 2022-09-20 Debiopharm Int Sa DRUG AND ITS USE FOR THE TREATMENT OF BACTERIAL INFECTIONS INVOLVING BIOFILM
BR112022012020A2 (en) 2019-12-19 2022-09-20 Debiopharm Int Sa NEW COMPOUNDS AND THEIR USE
PE20221575A1 (en) 2020-02-18 2022-10-06 Novo Nordisk As PHARMACEUTICAL FORMULATIONS
AU2022300316A1 (en) 2021-06-23 2024-02-08 Debiopharm International S.A. Novel compounds and their use

Family Cites Families (144)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3828068A (en) 1971-05-10 1974-08-06 Tenneco Chem ((substituted indazolyl)-n1-methyl)carbamates
US4154943A (en) 1977-12-29 1979-05-15 University Of Vermont Preparation of vincadifformine
FR2619111B1 (en) 1987-08-07 1991-01-11 Synthelabo (PIPERIDINYL-4) METHYL-2 TETRAHYDRO-1,2,3,4 9H-PYRIDO (3,4-B) INDOLE DERIVATIVES, THEIR PREPARATION AND THEIR THERAPEUTIC APPLICATION
CA2020437A1 (en) 1989-07-05 1991-01-06 Yoshihide Fuse Cinnamamide derivative
DE4126662A1 (en) 1991-08-13 1993-02-18 Boehringer Mannheim Gmbh NEW 3,5-DI-TERT.BUTYL-4-HYDROXYPHENYL DERIVATIVES, METHOD FOR THEIR PRODUCTION AND MEDICINAL PRODUCTS
HU210679B (en) 1991-11-21 1995-06-28 Richter Gedeon Vegyeszet Process for producing new tetrahydro-pyrido/3,4-b/indol derivatives and pharmaceutical compositions containing the same
FR2692575B1 (en) 1992-06-23 1995-06-30 Sanofi Elf NOVEL PYRAZOLE DERIVATIVES, PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM.
US5416193A (en) 1993-04-30 1995-05-16 Pfizer Inc. Coupling reagent and method
MA23420A1 (en) 1994-01-07 1995-10-01 Smithkline Beecham Corp BICYCLIC FIBRINOGEN ANTAGONISTS.
US5614551A (en) 1994-01-24 1997-03-25 The Johns Hopkins University Inhibitors of fatty acid synthesis as antimicrobial agents
AU702661B2 (en) 1994-06-29 1999-02-25 Smithkline Beecham Corporation Vitronectin receptor antagonists
US6176842B1 (en) 1995-03-08 2001-01-23 Ekos Corporation Ultrasound assembly for use with light activated drugs
US5989832A (en) 1995-04-21 1999-11-23 Microcide Pharmaceuticals, Inc. Method for screening for non-tetracycline efflux pump inhibitors
SK284962B6 (en) 1995-05-11 2006-03-02 Sandoz Ag 7-Acylamino-3-(hydrazono)methyl cephalosporins, preparation method thereof, intermediates for their preparation and pharmaceutical composition containing the same
US6057291A (en) 1995-06-02 2000-05-02 University Of British Columbia Antimicrobial cationic peptides
NZ512609A (en) 1996-02-29 2003-03-28 Fujisawa Pharmaceutical Co Synthetic sweeteners, their production and uses thereof
US6239154B1 (en) 1996-03-08 2001-05-29 Adolor Corporation Kappa agonist compounds pharmaceutical formulations and method of prevention and treatment of pruritus therewith
US6367985B1 (en) 1996-03-12 2002-04-09 Intellectual Property Company Optical connector using large diameter alignment features
US6451816B1 (en) 1997-06-20 2002-09-17 Klinge Pharma Gmbh Use of pyridyl alkane, pyridyl alkene and/or pyridyl alkine acid amides in the treatment of tumors or for immunosuppression
DE19624659A1 (en) 1996-06-20 1998-01-08 Klinge Co Chem Pharm Fab New pyridylalkene and pyridylalkanoic acid amides
US6503881B2 (en) 1996-08-21 2003-01-07 Micrologix Biotech Inc. Compositions and methods for treating infections using cationic peptides alone or in combination with antibiotics
US6995254B1 (en) 1996-08-28 2006-02-07 Affinium Pharmaceuticals, Inc. Polynucleotide encoding the enoyl-acyl carrier protein reductase of Staphylococcus aureus, FAB I
TR199900614T2 (en) 1996-09-20 1999-06-21 Meiji Seika Kaisha, Ltd. Crystalline substance Cefditoren pivoxil and its production.
US6521408B1 (en) 1997-09-25 2003-02-18 National Institute Of Agrobiological Sciences Method for assessing a function of a gene
DE19641437A1 (en) 1996-10-08 1998-04-09 Basf Ag 1,3-bis (N-lactamyl) propanes and their pharmaceutical and cosmetic use
DE19652239A1 (en) 1996-12-16 1998-06-18 Bayer Ag Use of 7- (2-oxa-5,8-diazabicyclo [4.3.0] non-8-yl) -quinolone and naphthyridonecarboxylic acid derivatives for the therapy of Helicobacter pylori infections and the associated gastroduodenal diseases
SI9600371B (en) 1996-12-18 2005-04-30 LEK, tovarna farmacevtskih in kemi�nih izdelkov, d.d. Ethylidene derivatives of tricyclic carbapenemes
AU6870098A (en) 1997-03-31 1998-10-22 Du Pont Merck Pharmaceutical Company, The Indazoles of cyclic ureas useful as hiv protease inhibitors
JP2001524951A (en) 1997-04-01 2001-12-04 トーマス ジュリアス ボロディー Methods and compositions for treating inflammatory bowel disease
US6406880B1 (en) 1997-05-02 2002-06-18 Integrated Research Technology, Llc Betaines as adjuvants to susceptibility testing and antimicrobial therapy
US6184363B1 (en) 1997-06-13 2001-02-06 Northwestern University Inhibitors of β-lactamases and uses therefor
US6207679B1 (en) 1997-06-19 2001-03-27 Sepracor, Inc. Antimicrobial agents uses and compositions related thereto
KR20010014105A (en) 1997-06-23 2001-02-26 가마쿠라 아키오 Prophylactic or therapeutic agent for diseases attributable to infection with helicobacters
AUPO758297A0 (en) 1997-06-27 1997-07-24 Rowe, James Baber Control of acidic gut syndrome
US6198000B1 (en) 1997-07-07 2001-03-06 Pfizer Inc. Intermediates useful in the synthesis of quinoline antibiotics
US6313153B1 (en) 1997-07-25 2001-11-06 Tsumura & Co. Compositions and methods for treating nephritis and inhibiting TGF -β related conditions using pyridylacrylamide derivatives
HN1998000106A (en) 1997-08-01 1999-01-08 Pfizer Prod Inc PARENTERAL COMPOSITIONS OF ALATROFLAXACINO
US5932743A (en) 1997-08-21 1999-08-03 American Home Products Corporation Methods for the solid phase synthesis of substituted indole compounds
GB9717804D0 (en) 1997-08-22 1997-10-29 Zeneca Ltd Chemical compounds
US6432444B1 (en) 1997-10-31 2002-08-13 New Horizons Diagnostics Corp Use of bacterial phage associated lysing enzymes for treating dermatological infections
UA85364C2 (en) 1997-10-31 2009-01-26 Сінгента Партісіпейшнс Аг Glyphosate-resistant sugar beet plant
WO1999024406A1 (en) 1997-11-07 1999-05-20 Schering Corporation Phenyl-alkyl-imidazoles as h3 receptor antagonists
SE9704404D0 (en) 1997-11-28 1997-11-28 Astra Ab New compounds
GB9725244D0 (en) 1997-11-29 1998-01-28 Zeneca Ltd Chemical compounds
DE19753298A1 (en) 1997-12-01 1999-06-02 Basf Ag Process for the preparation of solid dosage forms
HU230295B1 (en) 1998-01-07 2015-12-28 Meiji Seika Pharma Co., Ltd. Crystallographically stable amorphous cephalosporin compositions and process for producing the same
US6184380B1 (en) 1999-01-25 2001-02-06 Pfizer Inc. Process for preparing naphthyridones and intermediates
US6248343B1 (en) 1998-01-20 2001-06-19 Ethicon, Inc. Therapeutic antimicrobial compositions
PA8466701A1 (en) 1998-01-21 2000-09-29 Pfizer Prod Inc TROVAFLOXACINO MESYLATE TABLET
US6204279B1 (en) 1998-06-03 2001-03-20 Microcide Pharmaceuticals, Inc. Peptidomimetic efflux pump inhibitors
JP4726296B2 (en) 1998-02-27 2011-07-20 インスティチュート ストローマン アーゲー Matrix protein composition for wound healing
US6350738B1 (en) 1998-03-06 2002-02-26 Brigham Young University Steroid derived antibiotics
US6369049B1 (en) 1998-04-30 2002-04-09 Eli Lilly And Company Treatment of mastitis
DE19820801A1 (en) 1998-05-09 1999-11-25 Gruenenthal Gmbh Oral dosage form for gatifloxacin, providing reproducible decomposition time and drug release
DE19821039A1 (en) 1998-05-11 1999-11-18 Bayer Ag Production of (S,S)-8-benzyl-2,8-diazabicyclo(4.3.0)nonane useful as intermediate for antibiotic moxifloxacin
US6399629B1 (en) 1998-06-01 2002-06-04 Microcide Pharmaceuticals, Inc. Efflux pump inhibitors
US6428579B1 (en) 1998-07-01 2002-08-06 Brown University Research Foundation Implantable prosthetic devices coated with bioactive molecules
US6423741B1 (en) 1998-07-10 2002-07-23 Council Of Scientific And Industrial Research Anti-microbial composition and method for producing the same
GB9815567D0 (en) 1998-07-18 1998-09-16 Glaxo Group Ltd Antiviral compound
DK1101497T3 (en) 1998-08-04 2008-03-31 Schering Plough Animal Health Stabilizing oily preparations of tobicillin (beta-lactam antibiotic)
DE69932313T2 (en) 1998-08-21 2007-07-19 Senju Pharmaceutical Co., Ltd. AQUEOUS LIQUID PREPARATIONS
US6461607B1 (en) 1998-08-24 2002-10-08 Ganeden Biotech, Inc. Probiotic, lactic acid-producing bacteria and uses thereof
US6518487B1 (en) 1998-09-23 2003-02-11 Pioneer Hi-Bred International, Inc. Cyclin D polynucleotides, polypeptides and uses thereof
US6509327B1 (en) 1998-09-30 2003-01-21 Alcon Manufacturing, Ltd. Compositions and methods for treating otic, ophthalmic and nasal infections
US6395746B1 (en) 1998-09-30 2002-05-28 Alcon Manufacturing, Ltd. Methods of treating ophthalmic, otic and nasal infections and attendant inflammation
DE19851104C2 (en) 1998-11-06 2003-04-03 Huhtamaki Forchheim Process for producing a multilayer composite
TW526202B (en) 1998-11-27 2003-04-01 Shionogi & Amp Co Broad spectrum cephem having benzo[4,5-b]pyridium methyl group of antibiotic activity
JP4819223B2 (en) 1999-02-18 2011-11-24 ザ リージェンツ オブ ザ ユニバーシティ オブ カリフォルニア Phthalamide-lanthanide complexes for use as luminescent markers
US6235728B1 (en) 1999-02-19 2001-05-22 Bristol-Myers Squibb Company Water-soluble prodrugs of azole compounds
US6267985B1 (en) 1999-06-30 2001-07-31 Lipocine Inc. Clear oil-containing pharmaceutical compositions
US6294192B1 (en) 1999-02-26 2001-09-25 Lipocine, Inc. Triglyceride-free compositions and methods for improved delivery of hydrophobic therapeutic agents
US6248363B1 (en) 1999-11-23 2001-06-19 Lipocine, Inc. Solid carriers for improved delivery of active ingredients in pharmaceutical compositions
EP1159293A1 (en) 1999-03-03 2001-12-05 Princeton University Bacterial transglycosylases: assays for monitoring the activity using lipid ii substrate analogs and methods for discovering new antibiotics
US6495161B1 (en) 1999-03-09 2002-12-17 Vivorx, Inc. Cytoprotective biocompatible containment systems for biologically active materials and methods of making same
US6239113B1 (en) 1999-03-31 2001-05-29 Insite Vision, Incorporated Topical treatment or prevention of ocular infections
US6224579B1 (en) 1999-03-31 2001-05-01 The Trustees Of Columbia University In The City Of New York Triclosan and silver compound containing medical devices
WO2000059941A1 (en) 1999-04-08 2000-10-12 The General Hospital Corporation Purposeful movement of human migratory cells away from an agent source
CO5180550A1 (en) 1999-04-19 2002-07-30 Smithkline Beecham Corp FAB I INHIBITORS
US6290946B1 (en) 1999-05-13 2001-09-18 Geltex Pharmaceuticals, Inc. Anionic polymers as toxin binders and antibacterial agents
US6514535B2 (en) 1999-05-21 2003-02-04 Noveon Ip Holdings Corp. Bioadhesive hydrogels with functionalized degradable crosslinks
AR024077A1 (en) 1999-05-25 2002-09-04 Smithkline Beecham Corp ANTIBACTERIAL COMPOUNDS
CO5370679A1 (en) 1999-06-01 2004-02-27 Smithkline Beecham Corp FAB INHIBITORS 1
US6239141B1 (en) 1999-06-04 2001-05-29 Pfizer Inc. Trovafloxacin oral suspensions
CO5180605A1 (en) 1999-06-23 2002-07-30 Smithkline Beecham Corp INDOL COMPOUNDS
CA2282066C (en) 1999-06-29 2010-09-07 Smithkline Beecham Corporation Methods of use of quinolone compounds against atypical upper respiratory pathogenic bacteria
US6309663B1 (en) 1999-08-17 2001-10-30 Lipocine Inc. Triglyceride-free compositions and methods for enhanced absorption of hydrophilic therapeutic agents
US6500459B1 (en) 1999-07-21 2002-12-31 Harinderpal Chhabra Controlled onset and sustained release dosage forms and the preparation thereof
US6346391B1 (en) 1999-07-22 2002-02-12 Trustees Of Tufts College Methods of reducing microbial resistance to drugs
WO2001013956A2 (en) 1999-08-26 2001-03-01 Ganeden Biotech, Inc. Use of emu oil a carrier for antifungal, antibacterial, and antiviral medications
US6221859B1 (en) 1999-08-27 2001-04-24 Merck & Co., Inc. Carbapenem antibacterial compositions and methods of the treatment
US6174878B1 (en) 1999-08-31 2001-01-16 Alcon Laboratories, Inc. Topical use of kappa opioid agonists to treat otic pain
ES2282134T3 (en) 1999-09-11 2007-10-16 THE PROCTER & GAMBLE COMPANY POLYOXIALQUYLENE COPOLYMERS CONTAINING FLUID LIQUID VEHICLES.
KR20010101030A (en) 1999-09-17 2001-11-14 도리이 신이찌로 Antibacterial medicinal compositions
US6500463B1 (en) 1999-10-01 2002-12-31 General Mills, Inc. Encapsulation of sensitive components into a matrix to obtain discrete shelf-stable particles
ES2270874T3 (en) 1999-10-08 2007-04-16 Affinium Pharmaceuticals, Inc. FAB INHIBITORS I.
US6762201B1 (en) 1999-10-08 2004-07-13 Affinium Pharmaceuticals, Inc. Fab I inhibitors
WO2001026654A1 (en) 1999-10-08 2001-04-19 Smithkline Beecham Corporation Fab i inhibitors
NZ517706A (en) 1999-10-08 2004-01-30 Affinium Pharm Inc Fab I inhibitors
US6730684B1 (en) 1999-10-08 2004-05-04 Affinium Pharmaceuticals, Inc. Fab I inhibitors
CA2323008C (en) 1999-10-11 2005-07-12 Pfizer Inc. Pharmaceutically active compounds
WO2001029035A1 (en) 1999-10-19 2001-04-26 Sato Pharmaceutical Co., Ltd. 4-oxoquinolizine antimicrobials having 2-pyridone skeletons as the partial structure
US6951729B1 (en) 1999-10-27 2005-10-04 Affinium Pharmaceuticals, Inc. High throughput screening method for biological agents affecting fatty acid biosynthesis
ATE313318T1 (en) 1999-10-29 2006-01-15 Nektar Therapeutics DRY POWDER COMPOSITIONS WITH IMPROVED DISPERSITY
US6531291B1 (en) 1999-11-10 2003-03-11 The Trustees Of Columbia University In The City Of New York Antimicrobial activity of gemfibrozil and related compounds and derivatives and metabolites thereof
US6514986B2 (en) 2000-11-22 2003-02-04 Wockhardt Limited Chiral fluoroquinolone arginine salt forms
US6656703B1 (en) 1999-12-29 2003-12-02 Millennium Pharamaceuticals, Inc. High throughput screen for inhibitors of fatty acid biosynthesis in bacteria
US6372752B1 (en) 2000-02-07 2002-04-16 Genzyme Corporation Inha inhibitors and methods of use thereof
ES2179729B1 (en) 2000-03-23 2003-12-16 Dreiman Lab Farmaceuticos S A SOLID PHARMACEUTICAL FORM OF ORAL DISPERSABLE ADMINISTRATION IN WATER, WHICH INCLUDES RIFAMPICINE, ISONIAZIDE AND HYDROCHLORIDE PYRIDOXINE, PROCEDURE FOR OBTAINING AND FORM OF PRESENTATION OF SUCH PHARMACEUTICAL FORM.
WO2001072317A1 (en) 2000-03-28 2001-10-04 Council Of Scientific And Industrial Research Formulation comprising thymol useful in the treatment of drug resistant bacterial infections
CA2406215A1 (en) 2000-04-21 2001-11-01 Jay Francis Larrow Process for preparation of r-1-(aryloxy)propan-2-ol
AU2001282988B2 (en) 2000-07-26 2006-01-05 Atopic Pty Ltd Methods for treating atopic disorders
DE10037029A1 (en) 2000-07-27 2002-02-28 Kugelstrahlzentrum Aachen Gmbh Method and device for reshaping structural components
US6288239B1 (en) 2000-09-19 2001-09-11 Board Of Trustees Operating Michigan State University 5-trityloxymethyl-oxazolidinones and process for the preparation thereof
CA2423028A1 (en) 2000-09-21 2002-03-28 Cambridge Semiconductor Limited Semiconductor device and method of forming a semiconductor device
US6821746B2 (en) 2000-10-06 2004-11-23 Affinium Pharmaceuticals, Inc. Methods of screening for FabK antagonists and agonists
US7048926B2 (en) 2000-10-06 2006-05-23 Affinium Pharmaceuticals, Inc. Methods of agonizing and antagonizing FabK
CA2428191A1 (en) 2000-11-07 2002-05-30 Bristol-Myers Squibb Company Acid derivatives useful as serine protease inhibitors
AU2002232558A1 (en) 2000-12-12 2002-06-24 Corvas International, Inc. Compounds, compositions and methods for treatment of parasitic infections
US6388070B1 (en) 2001-01-05 2002-05-14 Orchid Chemicals & Pharmaceuticals Ltd. Thioester derivatives of thiazolyl acetic acid and their use in the preparation of cephalosporin compounds
US6495158B1 (en) 2001-01-19 2002-12-17 Lec Tec Corporation Acne patch
PA8539401A1 (en) 2001-02-14 2002-10-28 Warner Lambert Co QUINAZOLINAS AS INHIBITORS OF MMP-13
ES2320984T3 (en) 2001-04-06 2009-06-01 Affinium Pharmaceuticals, Inc. FAB INHIBITORS I.
US6503906B1 (en) 2002-02-21 2003-01-07 Ren-Jin Lee Method for optimizing ciprofloxacin treatment of anthrax-exposed patients according to the patient's characteristics
JPWO2003086396A1 (en) 2002-04-02 2005-08-18 株式会社ツムラ Phosphodiesterase IV inhibitors containing pyridylacrylic acid amide derivatives
AU2003250475A1 (en) 2002-08-13 2004-02-25 Warner-Lambert Company Llc 5,6-fused 3,4-dihydropyrimidine-2-one derivatives as matrix metalloproteinase inhibitors
CA2508792C (en) 2002-12-06 2013-02-05 Affinium Pharmaceuticals, Inc. Heterocyclic compounds, methods of making them and their use in therapy
JP4880448B2 (en) 2003-03-17 2012-02-22 アフィナム ファーマシューティカルズ，インコーポレーテッド Composition comprising a plurality of antibiotics and method of using the same
US7745625B2 (en) 2004-03-15 2010-06-29 Bristol-Myers Squibb Company Prodrugs of piperazine and substituted piperidine antiviral agents
ES2515101T3 (en) 2004-06-04 2014-10-29 Debiopharm International Sa Acrylamide derivatives as antibiotic agents
DE602006010979D1 (en) 2005-01-19 2010-01-21 Rigel Pharmaceuticals Inc PRODRUGS FROM 2,4-PYRIMIDIN DIAMIN COMPOUNDS AND THEIR USES
US20090156578A1 (en) 2005-12-05 2009-06-18 PAULS Henry 3-Heterocyclylacrylamide Compounds as Fab I Inhibitors and Antibacterial Agents
CN101415701A (en) * 2005-12-05 2009-04-22 Affinium医药公司 Heterocyclylacrylamide compounds as FABI inhibitors and antibacterial agents
WO2008009122A1 (en) 2006-07-20 2008-01-24 Affinium Pharmaceuticals, Inc. Acrylamide derivatives as fab i inhibitors
EP2420505A1 (en) 2006-11-21 2012-02-22 Rigel Pharmaceuticals, Inc. Prodrug salts of 2, 4- pyrimidinediamine compounds and their uses
EP2125802A4 (en) 2007-02-16 2014-08-20 Debiopharm Int Sa Salts, prodrugs and polymorphs of fab i inhibitors
WO2009003136A1 (en) 2007-06-26 2008-12-31 Rigel Pharmaceuticals, Inc. Substituted pyrimidine-2, 4 -diamines for treating cell proliferative disorders
DK2445502T4 (en) * 2009-06-25 2022-11-28 Alkermes Pharma Ireland Ltd HETEROCYCLIC COMPOUNDS FOR THE TREATMENT OF NEUROLOGICAL AND PSYCHOLOGICAL DISORDERS
JP5732453B2 (en) * 2009-06-25 2015-06-10 アルカーメス ファーマ アイルランド リミテッド Prodrugs of NH acidic compounds
UA108077C2 (en) 2009-07-02 2015-03-25 SYNTHESIS OF DINODIUM SALT N4- (2,2-DIMETHYL-4 - $ (DYHYDROPHOPHONOXY) METHYL] -3-OXO-5-PYRIDO $ 1,4] OXAZIN-6-YL) -2-FLUORINE 5-TRIMETHOXYPHENYL) -2,4-PYRIMIDINDIAMINE
CA2776849A1 (en) * 2009-11-18 2011-05-26 Fab Pharma S.A.S. Novel heterocyclic acrylamides and their use as pharmaceuticals
CA2802107A1 (en) 2010-06-11 2011-12-15 Affinium Pharmaceuticals, Inc. Compounds for treatment of bovine mastitis
CN102675311A (en) 2011-06-14 2012-09-19 苏春华 Fluoro-acrylamide derivative
EP2785715A1 (en) 2011-12-02 2014-10-08 Aurigene Discovery Technologies Limited Substituted pyridine derivatives as fabi inhibitors
SI2861608T1 (en) 2012-06-19 2019-08-30 Debiopharm International Sa Prodrug derivatives of (e)-n-methyl-n-((3-methylbenzofuran-2-yl)methyl)-3-(7-oxo-5,6,7,8-tetrahydro-1,8-naphthyridin-3-yl)acrylamide

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